IE970588A1 - Controlled release pharmaceutical compositions containing tiagabine - Google Patents

Controlled release pharmaceutical compositions containing tiagabine

Info

Publication number
IE970588A1
IE970588A1 IE19970588A IE970588A IE970588A1 IE 970588 A1 IE970588 A1 IE 970588A1 IE 19970588 A IE19970588 A IE 19970588A IE 970588 A IE970588 A IE 970588A IE 970588 A1 IE970588 A1 IE 970588A1
Authority
IE
Ireland
Prior art keywords
tiagabine
preparation
hours
preparation according
plasma concentration
Prior art date
Application number
IE19970588A
Inventor
Michelle Caulfield
Kenneth Iain Cumming
Maurice Joseph Anthony Clancy
Original Assignee
Elan Corp Plc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Elan Corp Plc filed Critical Elan Corp Plc
Priority to JP2000504859A priority Critical patent/JP2001511450A/en
Priority to DK98937738T priority patent/DK0991409T3/en
Priority to AT98937738T priority patent/ATE212550T1/en
Priority to PT98937738T priority patent/PT991409E/en
Priority to AU86436/98A priority patent/AU8643698A/en
Priority to ES98937738T priority patent/ES2172179T3/en
Priority to CA002299464A priority patent/CA2299464C/en
Priority to PCT/IE1998/000067 priority patent/WO1999006045A1/en
Priority to EP98937738A priority patent/EP0991409B1/en
Priority to DE69803670T priority patent/DE69803670T2/en
Publication of IE970588A1 publication Critical patent/IE970588A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Controlled release oral pharmaceutical preparations are provided which comprise a therapeutically effective amount of tiagabine or a pharmaceutically acceptable salt thereof dispersed in a rate controlling polymeric matrix comprising at least one rate controlling polymer. The preparation can be formulated into oral dosage forms such as tablets or multiparticulates which provide therapeutically effective plasma levels of tiagabine for a period of at least 12 hours, preferably 24 hours or more. The preparation can provide tiagabine mean plasma concentrations equal to or greater than 50% of the maximum plasma concentration for at least 10 hours, preferably 14 hours, most preferably 16 hours or more.

Description

Controlled release pharmaceutical compositions containing tiagabine Controlled release oral pharmaceutical preparations are provided which comprise a therapeutically effective amount of tiagabine or a pharmaceutically acceptable salt thereof dispersed in a rate controlling polymeric matrix comprising at least one rate controlling polymer. The preparation can be formulated into oral dosage forms such as tablets or multiparticulates which provide therapeutically effective plasma levels of tiagabine for a period of at least 12 hours, preferably 24 hours or more. The preparation can provide tiagabine mean plasma concentrations equal to or greater than 50% of the maximum plasma concentration for at least 10 hours, preferably 14 hours, most preferably 16 hours or more.
Controlled release pharmaceutical compositions containing tiagabine

Claims (27)

1. Claims:1. A controlled release oral pharmaceutical preparation comprising a therapeutically effective amount of tiagabine or a pharmaceutically acceptable salt thereof dispersed in a rate controlling polymeric matrix comprising at least one rate controlling polymer, which preparation provides therapeutically effective plasma levels of tiagabine for a period of at least 12 hours.
2. A preparation according to Claim 1, wherein the preparation releases tiagabine in vivo such that the duration over which the tiagabine plasma concentration is equal to or greater than 50% of the peak plasma concentration is 10 hours or greater.
3. A preparation according to Claim 1 or 2, wherein the in vivo maximum plasma concentration minus the minimum plasma concentration divided by the average plasma concentration taken over the effective period is less than 0.80.
4. A preparation according to any preceding claim, which provides a mean dissolution profile in aqueous media such that about 5 to 40% of the tiagabine is released after 1 hour; about 25 to 65% of the tiagabine is released after 4 hours; about 55 to 95% of the tiagabine is released after 10 hours and about 80 to 100% of the tiagabine is released after 22 hours.
5. A preparation according to any preceding claim, which provides therapeutic levels of tiagabine over a 24 hour period for oncedaily administration.
6. A preparation according to any preceding claim, wherein the duration over which the tiagabine plasma concentration is equal to or greater than 50% of the peak concentration is at least 15 hours.
7. A preparation according to any preceding claim, wherein the duration over which the tiagabine plasma concentration is equal to or greater than 50% of the peak concentration is at least 20 hours.
8. A preparation according to any one of Claims 3-7, wherein the in vivo maximum plasma concentration minus the minimum plasma concentration divided by the average plasma concentration taken over the effective period is less than 0.60.
9. A preparation according to any one of Claims 4-8, wherein the preparation provides a mean dissolution profile in aqueous media such that about 10 to 30% of the tiagabine is released after 1 hour; about 30 to 60% of the tiagabine is released after 4 hours; about 60 to 90% of the tiagabine is released after 10 hours and about 85 to 100% of the tiagabine is released after 22 hours.
10. A preparation according to any preceding claim, wherein the at least one rate controlling polymer is selected from hydroxypropylmethylcellulose, hydroxyalkylcellulose, alkylcellulose, poly(ethylene)oxide, carboxymethylcellulose, hydrophilic cellulose derivatives polyethylene glycols, polyvinylpyrrolidone, or mixtures thereof.
11. A preparation according to any preceding claim, wherein the at least one rate controlling polymer is selected from hydroxypropylmethylcellulose having a viscosity of about 100 to 100,000 cps, hydroxypropylcellulose having a molecular weight of about 80,000 to 1,150,000, ethylcellulose having a viscosity of about 3 to 110 cps and poly(ethylene)oxide having a molecular weight of about 100,000 to 7,000,000 or mixtures thereof.
12. A preparation according to any preceding claim, wherein the at least one rate controlling polymer comprises from about 5 to 75% by weight of the preparation.
13. A preparation according to any preceding claim, wherein the at least one rate controlling polymer comprises from about 20 to 50% by weight of the preparation.
14. A preparation according to any preceding claim, wherein the at least one rate controlling polymer comprises from about 30 to 45% by weight of the preparation.
15. A preparation according to any preceding claim, wherein the therapeutically effective amount of tiagabine or a pharmaceutically acceptable salt thereof is from about 5 to 100 mg.
16. A preparation according to any preceding claim, further comprising a diluent comprising from 10 to 90 % by weight of the preparation.
17. A preparation according to any preceding claim, wherein the rate controlling polymeric matrix is a hydrogel.
18. A preparation according to any preceding claim, wherein the at least one rate controlling polymer comprises from 19 to 31 % by weight of-a hydroxypropylmethylcellulose and from 9 to 15 % by weight of a hydroxypropylcellulose.
19. An oral dosage form suitable for once or twice daily administration containing a controlled release oral pharmaceutical preparation according to any one of Claims 1 to 18.
20. An oral dosage form according to Claim 19, which is in the form of tablets.
21. An oral dosage form according to Claim 19, which is in the form of pellets or mini-tablets.
22. An oral dosage form according to Claim 19, which is in the form of a blend of at least two populations of pellets or mini-tablets, wherein each population has a different controlled-release dissolution profile.
23. An oral dosage form according to any one of Claims 19 to 22, further comprising a controlled release polymer layer coated on the preparation.
24. An oral dosage form according to any one of Claims 19 to 23, further comprising a light-protective or cosmetic film coated on the preparation.
25. An oral dosage form according to Claim 21 or Claim 22, further comprising immediate release pellets or mini-tablets containing tiagabine or a pharmaceutically acceptable salt thereof.
26. A controlled release oral pharmaceutical preparation according to Claim 1, substantially as hereinbefore described and exemplified.
27. An oral dosage form according to Claim 19, substantially as hereinbefore exemplified. ANNE RYAN & CO. Agents for the Applicants 1/2
IE19970588A 1997-08-01 1997-08-08 Controlled release pharmaceutical compositions containing tiagabine IE970588A1 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
JP2000504859A JP2001511450A (en) 1997-08-01 1998-07-30 Controlled release pharmaceutical composition containing tiagabine
DK98937738T DK0991409T3 (en) 1997-08-01 1998-07-30 Pharmaceutical controlled release tenagabine-containing preparations
AT98937738T ATE212550T1 (en) 1997-08-01 1998-07-30 MEDICINAL PREPARATIONS CONTAINING TIAGABINE WITH CONTROLLED ADMINISTRATION OF ACTIVE INGREDIENTS
PT98937738T PT991409E (en) 1997-08-01 1998-07-30 COMPOSITIONS OF CONTROLLED LIBERATION CONTAINING TIAGABINE
AU86436/98A AU8643698A (en) 1997-08-01 1998-07-30 Controlled release pharmaceutical compositions containing tiagabine
ES98937738T ES2172179T3 (en) 1997-08-01 1998-07-30 PHARMACEUTICAL COMPOSITIONS OF CONTROLLED RELEASE CONTAINING THIAGABINE.
CA002299464A CA2299464C (en) 1997-08-01 1998-07-30 Controlled release pharmaceutical compositions containing tiagabine
PCT/IE1998/000067 WO1999006045A1 (en) 1997-08-01 1998-07-30 Controlled release pharmaceutical compositions containing tiagabine
EP98937738A EP0991409B1 (en) 1997-08-01 1998-07-30 Controlled release pharmaceutical compositions containing tiagabine
DE69803670T DE69803670T2 (en) 1997-08-01 1998-07-30 MEDICINE PREPARATIONS WITH TIAGABINE WITH CONTROLLED ACTIVE SUBSTANCE ADMINISTRATION

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US5443297P 1997-08-01 1997-08-01

Publications (1)

Publication Number Publication Date
IE970588A1 true IE970588A1 (en) 2000-08-23

Family

ID=21991024

Family Applications (1)

Application Number Title Priority Date Filing Date
IE19970588A IE970588A1 (en) 1997-08-01 1997-08-08 Controlled release pharmaceutical compositions containing tiagabine

Country Status (3)

Country Link
US (1) US6399100B1 (en)
IE (1) IE970588A1 (en)
ZA (1) ZA986889B (en)

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US20030091630A1 (en) * 2001-10-25 2003-05-15 Jenny Louie-Helm Formulation of an erodible, gastric retentive oral dosage form using in vitro disintegration test data
US20030152622A1 (en) * 2001-10-25 2003-08-14 Jenny Louie-Helm Formulation of an erodible, gastric retentive oral diuretic
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US8075872B2 (en) 2003-08-06 2011-12-13 Gruenenthal Gmbh Abuse-proofed dosage form
US20070048228A1 (en) 2003-08-06 2007-03-01 Elisabeth Arkenau-Maric Abuse-proofed dosage form
DE10336400A1 (en) 2003-08-06 2005-03-24 Grünenthal GmbH Anti-abuse dosage form
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DE102004032049A1 (en) * 2004-07-01 2006-01-19 Grünenthal GmbH Anti-abuse, oral dosage form
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EA201400172A1 (en) 2011-07-29 2014-06-30 Грюненталь Гмбх SUSTAINABLE TO DESTRUCTION TABLET THAT PROVIDES IMMEDIATE RELEASE OF MEDICINES
AU2012292418B2 (en) 2011-07-29 2017-02-16 Grunenthal Gmbh Tamper-resistant tablet providing immediate drug release
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WO2014191396A1 (en) 2013-05-29 2014-12-04 Grünenthal GmbH Tamper resistant dosage form with bimodal release profile
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Also Published As

Publication number Publication date
US6399100B1 (en) 2002-06-04
ZA986889B (en) 1999-12-28

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MM4A Patent lapsed